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Assay Detail

CHEMBL648765

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Tested for inhibition of [125I]- AII specific binding to rat mesenteric arteries, expressed as IC50
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Type-1 angiotensin II receptor B (CHEMBL263)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

A potent long-acting imidazole-5-acrylic acid angiotensin II AT-1 receptor antagonist
Weinstock J, Hill DT, Keenan RM, Franz RG, Gaitanopoulos DE, Girard GR, Eggleston DS, Aiyar N, Griffin E, Ohlstein E, Brooks DP, Gellai M, Frederickson TA, Weidley EF, Edwards RM
Bioorg Med Chem Lett (1994) 4 : 23 -28
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 8.67 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL317343 1 9.80
CHEMBL813 EPROSARTAN 4.0 1 9.00
CHEMBL57309 1 8.98
CHEMBL37679 1 8.84
CHEMBL97533 1 7.93
CHEMBL56574 1 7.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL317343 IC50 = 0.16 nM 9.80
CHEMBL813 EPROSARTAN IC50 = 1.0 nM 9.00
CHEMBL57309 IC50 = 1.04 nM 8.98
CHEMBL37679 IC50 = 1.45 nM 8.84
CHEMBL97533 IC50 = 11.8 nM 7.93
CHEMBL56574 IC50 = 35.4 nM 7.45